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Showing 1–8 of 8 results
Advanced filters: Author: Harald Weinstabl Clear advanced filters

  • TEAD transcription factors are critical effectors and druggable sites of the Hippo pathway in cancer, however, the development of small molecule inhibitors and degraders remains underexplored. Here, the authors identify and characterize bifunctional IAP-based degraders targeting TEAD1 via a lipid pocket and recruit different members of the inhibitor of apoptosis proteins (IAPs) family, offering a comprehensive toolkit for structural, biophysical and cellular profiling.

    • Nishma Gupta
    • Nicole Trainor
    • Michael J. Roy
    ResearchOpen Access
    Communications Chemistry
    P: 1-23

  • Citizen science taps the efforts of non-experts. Here, authors describe Drugit, an extension of the crowdsourcing game Foldit, and its use in designing a non-peptide binder of Von Hippel Lindau E3 ligase for use with proteolysis targeting chimeras.

    • Thomas Scott
    • Christian Alan Paul Smethurst
    • Rocco Moretti
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-11

  • Antimicrobial resistance is a global health threat and the development of alternative strategies to overcome it is of high interest. Here, the authors report proteolysis targeting chimeras active in bacteria (BacPROTACs) that bind to ClpC1, a component of the mycobacterial protein degradation machinery, and apply them for targeting a range of mycobacterial strains, including antibiotic-resistant ones.

    • Lukas Junk
    • Volker M. Schmiedel
    • Guido Boehmelt
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-15

  • Protein degraders are an emerging drug modality; however, their properties lie beyond typical drug-like space. Here the authors report optimisation via structure-based exit vector and linker design towards the VHL-recruiting PROTAC ACBI2, an orally bioavailable and selective degrader of SMARCA2.

    • Christiane Kofink
    • Nicole Trainor
    • William Farnaby
    ResearchOpen Access
    Nature Communications
    Volume: 13, P: 1-15

  • Pharmacological probes are important tools for exploring disease biology and discovering new therapies. Often molecules of insufficient quality are used instead, leading to spurious and misleading results. The Boehringer Ingelheim open innovation portal opnMe.com addresses this deficiency by sharing extensively validated pharmacological probes with the scientific community.

    • Andreas Gollner
    • Markus Köster
    • Florian Montel
    Comments & Opinion
    Nature Reviews Drug Discovery
    Volume: 21, P: 475-476